ArticleJournal of cellular physiology2008
Topical administration of a multi-targeted kinase inhibitor suppresses choroidal neovascularization and retinal edema.
Article in Journal of cellular physiology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
25 citing papers in PubMed, 68 citations in OpenAlex.
- Challenges and opportunities of developing small-molecule therapies for age-related macular degeneration.Archives of pharmacal research · 2024Review
- Understanding the Impact of Polyunsaturated Fatty Acids on Age-Related Macular Degeneration: A Review.International journal of molecular sciences · 2024Review
- Overcoming Treatment Challenges in Posterior Segment Diseases with Biodegradable Nano-Based Drug Delivery Systems.Pharmaceutics · 2023Review
- Topical Drug Delivery to the Posterior Segment of the Eye.Pharmaceutics · 2022Review
- Topical Drug Delivery to the Posterior Segment of the Eye: Addressing the Challenge of Preclinical to Clinical Translation.Pharmaceutical research · 2018Review
- The HIF-1 antagonist acriflavine: visualization in retina and suppression of ocular neovascularization.Journal of molecular medicine (Berlin, Germany) · 2017Article
- Antiangiogenic effects of topically administered multiple kinase inhibitor, motesanib (AMG 706), on experimental choroidal neovascularization in mice.Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics · 2015Article
- Seeing through VEGF: innate and adaptive immunity in pathological angiogenesis in the eye.Trends in molecular medicine · 2015Review
- Characteristic findings of optical coherence tomography in retinal angiomatous proliferation.Korean journal of ophthalmology : KJO · 2013Article
- Topical antiangiogenic SRPK1 inhibitors reduce choroidal neovascularization in rodent models of exudative AMD.Investigative ophthalmology & visual science · 2013Article
- Topical pazopanib blocks VEGF-induced vascular leakage and neovascularization in the mouse retina but is ineffective in the rabbit.Investigative ophthalmology & visual science · 2013Article
- Diabetic macular edema: current and emerging therapies.Middle East African journal of ophthalmology · 2012Article
- An anti-inflammatory role of VEGFR2/Src kinase inhibitor in herpes simplex virus 1-induced immunopathology.Journal of virology · 2011Article
- Optical coherence tomography: history, current status, and laboratory work.Investigative ophthalmology & visual science · 2011Review
- Emerging therapeutic approaches in the management of retinal angiogenesis and edema.Journal of molecular medicine (Berlin, Germany) · 2011Review
- SU5416 induces premature senescence in endothelial progenitor cells from patients with age-related macular degeneration.Molecular vision · 2011Article
- Effect of polyphenols on oxidative stress and mitochondrial dysfunction in neuronal death and brain edema in cerebral ischemia.International journal of molecular sciences · 2011Review
- Age-related macular degeneration.Clinical ophthalmology (Auckland, N.Z.) · 2011Article
- Ophthalmic drug delivery systems for the treatment of retinal diseases: basic research to clinical applications.Investigative ophthalmology & visual science · 2010Article
- Digoxin inhibits retinal ischemia-induced HIF-1alpha expression and ocular neovascularization.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2010Article
Corrections and comments
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Authors and funding
16 authors at 2 institutions in 1 country.
Funding
Abstract
Age-related macular degeneration, diabetic retinopathy, and retinal vein occlusions are complicated by neovascularization and macular edema. Multi-targeted kinase inhibitors that inhibit select growth factor receptor tyrosine kinases and/or components of their down-stream signaling cascades (such as Src kinases) are rationale treatment strategies for these disease processes. We describe the discovery and characterization of two such agents. TG100572, which inhibits Src kinases and selected receptor tyrosine kinases, induced apoptosis of proliferating endothelial cells in vitro. Systemic delivery of TG100572 in a murine model of laser-induced choroidal neovascularization (CNV) caused significant suppression of CNV, but with an associated weight loss suggestive of systemic toxicity. To minimize systemic exposure, topical delivery of TG100572 to the cornea was explored, and while substantial levels of TG100572 were achieved in the retina and choroid, superior exposure levels were achieved using TG100801, an inactive prodrug that generates TG100572 by de-esterification. Neither TG100801 nor TG100572 were detectable in plasma following topical delivery of TG100801, and adverse safety signals (such as weight loss) were not observed even with prolonged dosing schedules. Topical TG100801 significantly suppressed laser-induced CNV in mice, and reduced fluorescein leakage from the vasculature and retinal thickening measured by optical coherence tomography in a rat model of retinal vein occlusion. These data suggest that TG100801 may provide a new topically applied treatment approach for ocular neovascularization and retinal edema.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.